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February 19, 2026Assay and Drug Development Technologies0 citationsOpen Access

Identifying Kir2.1 Inhibitors Through High-Throughput Screening

Identification of Kir2.1 Inhibitors from a High-Throughput Screen

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Authors

JBJacob L. BouchardPHPatricia Van HornYNYu Nishio

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Overview

High-throughput screening uncovers Kir2.1 inhibitors, suggesting new avenues for drug development.

Key Points

  • This research aims to identify novel inhibitors of the Kir2.1 potassium channel using high-throughput screening.
  • Conducted a high-throughput screen of over 20,000 compounds from a chemical biology discovery collection.
  • Verified 48 hits and identified six novel chemical scaffolds.
  • Selected VU0523203 and VU0606851 for medicinal chemistry optimization.
  • Discovered VU6073995, a new compound with modest potency at Kir2.1.
  • VU6073995 shows improved DMPK properties compared to existing compounds like ML133.

Cite This Study

Bouchard et al. (2026) studied this question.

synapsesocial.com/papers/6996a84cecb39a600b3eed56https://doi.org/10.1177/1540658x261415763
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